Evaluation of Potential Herb-drug Interactions between Oseltamivir and Commonly Used Anti-influenza Chinese Medicinal Herbs
Refereed conference paper presented and published in conference proceedings


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AbstractOseltamivir (O) is a potent and selective inhibitor of the neuraminidases glycoprotein. Our preliminary studies suggested that co-administration of YinQiaoSan and SangJuYin with O in rats would inhibit the transformation of O to oseltamivir acid (OA). To clarify if such herb-drug interactions are prevalent between O and commonly used anti-influenza Chinese medicinal herbs, eight herbs and ten marker components from these eight herbs are selected for the screening of potential herb-drug interactions in rats.

To screen potential inhibition of herbs/herbal components on O hydrolysis, O was incubated with herbs/herbal components in diluted rat plasma, microsomes and human recombinant carboxylesterase 1 (hCE1) under optimized conditions. MDCK-WT and MDCK-MDR1 cell lines were utilized to identify potential modification of herbs/herbal components on P-gp mediated transport of O. Caco-2 cell monolayer model was used to study the effect of herbs/herbal components on the uptake of O via PEPT1. Modification on OAT3 mediated transport by herbs/herbal components was verified by the uptake of O in HEK293-MOCK/HEK293-OAT3 cells.

Our results demonstrated that Fructus Forsythiae and Fructus Arctii could extensively inhibit the hydrolysis of O (>97%). Herbal components including Baicalein, Wogonin and Arctiin also showed significant inhibition on the hydrolysis of O (>50%). In addition, Epigoitrin showed strong inhibition of O hydrolysis in rat liver microsomes and hCE1. Our developed in vitro screening model for transport of O indicated that i) Baicalein, Glycyrrhizic acid and Radix et Rhizoma Glycyrrhizae could inhibit the P-gp mediated efflux of O; ii) no OAT3-mediated transport and limited uptake through PEPT1 transporter were observed for O. Anti-virus effects were evaluated using plaque reduction assay for H1N1 and H3N2 viruses, which found no significant inhibition on the virus plaque reduction of O by the studied herbal components. Potential in vivo pharmacokinetic and pharmacodynamic interaction between O and the selected herb of Radix Scutellariae (RS) with the most potent impact on the absorption and metabolism of O were carried out in rats. It was found that RS could only inhibit the hydrolysis of O with no influence on its overall anti-virus effects.

In summary, the selected commonly used anti-influenza herbs and their marker components could cause potential pharmacokinetic but not pharmacodynamic herb-drug interactions. Further in vivo evaluation on human is warranted for its potential clinical impact.
All Author(s) ListYufeng Zhang, Chunming Lyu, Qian Wang, Chenrui Li, Apple Yeung, Kay Sheung Paul Chan, Zhong Zuo
Name of ConferenceHealth Research Symposium 2017
Start Date of Conference16/06/2017
End Date of Conference16/06/2017
Place of ConferenceHong Kong
Country/Region of ConferenceHong Kong
Year2017
LanguagesEnglish-United States

Last updated on 2018-02-10 at 09:44